Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor §

…, NM King, M Prabu-Jeyabalan…

文献索引：Surleraux, Dominique L. N. G.; Tahri, Abdellah; Verschueren, Wim G.; Pille, Geert M. E.; De Kock, Herman A.; Jonckers, Tim H. M.; Peeters, Anik; De Meyer, Sandra; Azijn, Hilde; Pauwels, Rudi; De Bethune, Marie-Pierre; King, Nancy M.; Prabu-Jeyabalan, Moses; Schiffer, Celia A.; Wigerinck, Piet B. T. P. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1813 - 1822

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被引用次数: 213

摘要

The screening of known HIV-1 protease inhibitors against a panel of multi-drug-resistant viruses revealed the potent activity of TMC126 on drug-resistant mutants. In comparison to amprenavir, the improved affinity of TMC126 is largely the result of one extra hydrogen bond to the backbone of the protein in the P2 pocket. Modification of the substitution pattern on the phenylsulfonamide P2'substituent of TMC126 created an interesting SAR, with the close ...